SANT-1

製品コードS7092 バッチS709201

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₃H₂₇N₅

分子量

373.49

CAS No.

304909-07-7

Solubility (25°C)*

体外

DMSO

21 mg/mL (56.22 mM)

Ethanol

20 mg/mL (53.54 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.050mg/ml (2.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 21 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.050mg/ml (2.81mM)	Taking the 1 mL working solution as an example, add 50 μL of 21 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	SANT-1 directly binds to Smoothened (Smo) receptor with K_d of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.
in vitro	SANT-1 inhibits wild type and oncogenic Smo with equal potency. This compound counteracts SAG-induced pathway activation in Shh-LIGHT2 cells. It is able to block BODIPY-cyclopamine binding to Smo-expressing cells, but this chemical is unable to inhibit completely this association to background levels. This suggests that their interactions with Smo may alter its affinity for cyclopamine rather than compete directly for cyclopamine binding. The compound blocks pathway activation in SmoA1-LIGHT2 cells with potencies similar to those observed in the Shh-LIGHT2 assay. It has disparate inhibitory activities in the Shh-LIGHT2 and BODIPY-cyclopamine assays and is unusually potent at blocking SAG-mediated pathway activation.^[1] This compound efficiently inhibited cyclopamine- and jervine- induced translocation of Smo to the primary cilium. It inhibits PKA stimulation of Smo trafficking to the proximal cilium.^[2]
特徴	Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists.

製品説明

SANT-1 directly binds to Smoothened (Smo) receptor with K_d of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.

in vitro

SANT-1 inhibits wild type and oncogenic Smo with equal potency. This compound counteracts SAG-induced pathway activation in Shh-LIGHT2 cells. It is able to block BODIPY-cyclopamine binding to Smo-expressing cells, but this chemical is unable to inhibit completely this association to background levels. This suggests that their interactions with Smo may alter its affinity for cyclopamine rather than compete directly for cyclopamine binding. The compound blocks pathway activation in SmoA1-LIGHT2 cells with potencies similar to those observed in the Shh-LIGHT2 assay. It has disparate inhibitory activities in the Shh-LIGHT2 and BODIPY-cyclopamine assays and is unusually potent at blocking SAG-mediated pathway activation.^[1]

This compound efficiently inhibited cyclopamine- and jervine- induced translocation of Smo to the primary cilium. It inhibits PKA stimulation of Smo trafficking to the proximal cilium.^[2]

特徴

Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists.

プロトコル(参考用のみ)

キナーゼアッセイ	Small Molecule Screens for Hh Pathway Modulators
キナーゼアッセイ	Shh-N (N-terminal fragment of Shh without cholesterol modification)-conditioned medium is obtained from an HEK 293 cell line stably transfected with Shh-N expression and neomycin resistance constructs. The Shh-N-producing HEK 293 cells are grown to 80% confluency in DMEM containing 10% (vol/vol) FBS and 400 μg/ml G418. The medium then is replaced with DMEM containing 2% (vol/vol) FBS, and after 1 day of growth, the medium is collected and filtered through a 0.22-μm membrane. Control medium is obtained from HEK 293 cells. Shh-LIGHT2 cells are then cultured to confluency in 96-well plates and treated with this compound (0.714 μg/mL; ≈2 μM compound in each well) in the presence of either Shh-N-conditioned medium or HEK 293 control medium (1:25 dilution into DMEM containing 0.5% bovine calf serum). After incubating the treated cells for 30 h at 37°C, cellular firefly and Renilla luciferase activities are measured.
細胞アッセイ	細胞株	Cell-free assays
	濃度	20 nM
	反応時間
	実験の流れ
動物実験	動物モデル	Swiss albino male mice
	投薬量	3.3 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/12391318/
https://pubmed.ncbi.nlm.nih.gov/19365551/
https://pubmed.ncbi.nlm.nih.gov/19421011/

カスタマーフィードバック

: , , Oncotarget, 2017, 8(40): 67891-67903

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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Compound Tongluo Decoction inhibits endoplasmic reticulum stress-induced ferroptosis and promoted angiogenesis by activating the Sonic Hedgehog pathway in cerebral infarction [ J Ethnopharmacol, 2021, S0378-8741(21)00863-1]	PubMed: 34536518

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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